| Identification | Back Directory | [Name]
5-Thiazolecarboxamide, 4-(cyclopropylmethoxy)-N-methyl-2-[2-[[2-[[2-[(1,2,3,4-tetrahydro-9-acridinyl)amino]ethyl]amino]acetyl]amino]-4-pyridinyl]- | [CAS]
2412364-73-7 | [Synonyms]
AChE/GSK-3β-IN-1
5-Thiazolecarboxamide, 4-(cyclopropylmethoxy)-N-methyl-2-[2-[[2-[[2-[(1,2,3,4-tetrahydro-9-acridinyl)amino]ethyl]amino]acetyl]amino]-4-pyridinyl]- | [Molecular Formula]
C31H35N7O3S | [MOL File]
2412364-73-7.mol | [Molecular Weight]
585.72 |
| Hazard Information | Back Directory | [Uses]
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research[1]. | [in vivo]
AChE/GSK-3β-IN-1 (compound GT15) (15 mg/kg,; p.o.; ICR male mice) has a function of improving memory and cognition in mice[1]. | Animal Model: | ICR male mice[1] | | Dosage: | 15 mg/kg | | Administration: | Oral administration | | Result: | Improved the cognitive impairment of the mice. |
| [References]
[1] Jiang X, et, al. Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease. Eur J Med Chem. 2020 Dec 1;207:112751. DOI:10.1016/j.ejmech.2020.112751 |
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